The invention is directed to sterolin compounds and their use for medicinal or therapeutic purposes.
Sterolins are compounds which occur frequently in nature in plants and microorganisms and their function in plants has not yet been established. Sterolins are glycosides of phytosterols including cholesterol and sterol type tetracyclic triterpenes as for example lanosterol and cycloartenol. About 100 different natural phytosterols have been found so far; of them many occur very rarely, as for example, lanosterol, while others occur frequently in plants but then only in small amounts as, for example, cycloartenol or cholesterol or some of them occur only in specific plants or plant families. However, several of these compound, also occur in various plants in relatively large amounts, as for example, sitosterol and campesterol as well as stigmasterol. Of these last mentioned compounds sitosterol particularly occurs most frequently.
The phytosterols correspond predominantly to the following general formula: ##STR1## in which R.sup.1, R.sup.2 and R.sup.3 are hydrogen atoms or methyl groups and in which R.sup.4 can be a hydrogen atom or a methyl, ethyl, methylene or ethylidene group. Furthermore, double bonds can be present at various positions of the basic skeleton including the side chain.
It has already been established that these phytosterols are present in most plants as steryl glycosides, i.e., as sterolins and as their esters. An exception appears to be the tetracyclic triterpene sterols which do not seem to exist in nature as glycosides. The most common sterolins are monoglycosides, although a few diglycosides have been described. The most common sugar is D-glucose usually by means of which is joined to the sterol via the 3-.beta.-hydroxy group, usually by means of an equatorial or .beta.-glucoside bond. Other monosaccharides found in these compounds are mannose, galactose, arabinose and xylose. Sterolin esters are derived from monobasic carboxylic acids, e.g., palmitic acid.
Plants may contain specific sterols but usually they carry a mixture of different, sterols, sterol esters, sterolins and sterolin esters.
Sterols and sterol esters have not generally been used in medical practice except for specific phytosterols such as sitosterol and fucosterol which are employed; in very high doses of abnormally high serum cholesterol levels.
Sterolins and sterolin esters have already been described as biologically active. Reference to this is found in the German OS 21 13 215 and 23 12 285 corresponding to British patents 1,298,047 and 1,417,272. Furthermore, the German OS 23 03 247 and 21 13 215 corresponding to British patents 1,365,661 and 1,298,047 and the German OS 24 58 890 have disclosed the production of pharmaceutical specialities containing sterolin compounds. The entire disclosures of these German Inspection Applications and British patents are hereby incorporated by reference and they help to define the subject matter.
In these publications reference is made to the fact that sterolin compounds exhibit practically no toxicity and they can therefore be used in the treatment of various diseases. According to these publications, sterolins were also employed in the treatment of gout and arthritis.
Surprisingly and completely unexpected it has now been established that large doses of sterolins or sterolin esters may precipitate gout-like symptoms on predisposed patient.